3d5v

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{{Seed}}
 
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[[Image:3d5v.png|left|200px]]
 
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==Crystal structure of an activated (Thr->Asp) Polo-like kinase 1 (Plk1) catalytic domain.==
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The line below this paragraph, containing "STRUCTURE_3d5v", creates the "Structure Box" on the page.
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<StructureSection load='3d5v' size='340' side='right'caption='[[3d5v]], [[Resolution|resolution]] 2.40&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[3d5v]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Danio_rerio Danio rerio]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3D5V OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3D5V FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.4&#8491;</td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3d5v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3d5v OCA], [https://pdbe.org/3d5v PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3d5v RCSB], [https://www.ebi.ac.uk/pdbsum/3d5v PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3d5v ProSAT]</span></td></tr>
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{{STRUCTURE_3d5v| PDB=3d5v | SCENE= }}
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/Q6DRK7_DANRE Q6DRK7_DANRE]
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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/d5/3d5v_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=3d5v ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Polo-like kinase 1 (Plk1) is a member of a family of serine/threonine kinases involved in the regulation of cell-cycle progression and cytokinesis and is an attractive target for the development of anticancer therapeutics. A zebrafish homolog of the human Plk1 (hPlk1) kinase domain (KD) was identified that can be expressed in large quantities in bacteria and crystallizes readily, whether in a wild-type form or as a variant containing the activating Thr196--&gt;Asp substitution, in one space group and under similar conditions both in the absence and presence of active-site compounds. This construct was validated by testing a panel of hPlk1 inhibitors against human and zebrafish proteins and it was shown that the selected small molecules inhibited the homologs with a high degree of correlation. Crystal structures of ligand-free wild-type and activated zebrafish Plk1 (zPlk1) KDs revealed the organization of the secondary structural elements around the active site and demonstrated that the activation segment was disordered in the activated form of the domain but possessed a well defined secondary structure in the wild-type enzyme. The cocrystal structure of wild-type zPlk1 KD with ADP documented the hydrolysis of ATP and revealed the phosphorylation site. The cocrystal structure of the activated KD with wortmannin, a covalent inhibitor of Plk1 and PI3 kinases, showed the binding mode of the small molecule to the enzyme and may facilitate the design of more potent Plk1 inhibitors. The work presented in this study establishes the zPlk1 KD as a useful tool for rapid low- and high-throughput structure-based screening and drug discovery of compounds specific for this mitotic target.
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===Crystal structure of an activated (Thr->Asp) Polo-like kinase 1 (Plk1) catalytic domain.===
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Structures of the wild-type and activated catalytic domains of Brachydanio rerio Polo-like kinase 1 (Plk1): changes in the active-site conformation and interactions with ligands.,Elling RA, Fucini RV, Romanowski MJ Acta Crystallogr D Biol Crystallogr. 2008 Sep;64(Pt 9):909-18. Epub 2008, Aug 13. PMID:18703838<ref>PMID:18703838</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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The line below this paragraph, {{ABSTRACT_PUBMED_18703838}}, adds the Publication Abstract to the page
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<div class="pdbe-citations 3d5v" style="background-color:#fffaf0;"></div>
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(as it appears on PubMed at http://www.pubmed.gov), where 18703838 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_18703838}}
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__TOC__
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</StructureSection>
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==About this Structure==
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3D5V is a 1 chain structure of sequence from [http://en.wikipedia.org/wiki/Danio_rerio Danio rerio]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3D5V OCA].
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==Reference==
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<ref group="xtra">PMID:18703838</ref><references group="xtra"/>
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[[Category: Danio rerio]]
[[Category: Danio rerio]]
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[[Category: Polo kinase]]
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[[Category: Large Structures]]
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[[Category: Elling, R A.]]
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[[Category: Elling RA]]
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[[Category: Fucini, R V.]]
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[[Category: Fucini RV]]
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[[Category: Romanowski, M J.]]
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[[Category: Romanowski MJ]]
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[[Category: Catalytic domain]]
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[[Category: Kinase]]
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[[Category: Plk1]]
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[[Category: Polo-like kinase 1]]
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[[Category: Small-molecule inhibitor]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Feb 18 07:59:35 2009''
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Current revision

Crystal structure of an activated (Thr->Asp) Polo-like kinase 1 (Plk1) catalytic domain.

PDB ID 3d5v

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